Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Anti-inflammatory medicaments

a technology of anti-inflammatory and anti-inflammatory drugs, which is applied in the field of anti-inflammatory medicaments, can solve the problems of lack of selectivity, insufficient therapeutic windows to achieve maximum efficacy, and the method and strategy by which the pharmaceutical industry sets about to develop small molecule therapeutics has not significantly advanced, so as to achieve greater propensity, lesser propensity to interact, and greater propensity

Inactive Publication Date: 2007-08-16
DECIPHERA PHARMA LLC
View PDF10 Cites 95 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about new compounds and methods for treating inflammatory conditions. The compounds have specific formulas and can be used to treat various inflammatory conditions such as arthritis, lupus erythematosus, and Crohn's disease. The compounds have the ability to inhibit the production of inflammatory cytokines and can be used in combination with other compounds to further enhance their effectiveness. The invention also includes methods for making the compounds and using them to treat inflammatory conditions.

Problems solved by technology

Despite the wealth of information that the human genome and its proteins are providing, particularly in the area of conformational control of protein function, the methodology and strategy by which the pharmaceutical industry sets about to develop small molecule therapeutics has not significantly advanced beyond using native protein active sites for binding to small molecule therapeutic agents.
Because these native pockets are used broadly by many other proteins within protein families, drugs which interact with them are often plagued by lack of selectivity and, as a consequence, insufficient therapeutic windows to achieve maximum efficacy.
Side effects and toxicities continue to be a major reason for the high attrition rate seen within the drug development process.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Anti-inflammatory medicaments
  • Anti-inflammatory medicaments
  • Anti-inflammatory medicaments

Examples

Experimental program
Comparison scheme
Effect test

examples

[0240] The following examples set forth preferred methods in accordance with the invention. It is to be understood, however, that these examples are provided by way of illustration and nothing therein should be taken as a limitation upon the overall scope of the invention.

[0241] [Boc-sulfamide] aminoester (Reagent AA), 1,5,7,-trimethyl-2,4-dioxo-3-aza-bicyclo[3.3.1]nonane-7-carboxylic acid (Reagent BB), and Kemp acid anhydride (Reagent CC) was prepared according to literature procedures. See Askew et. al J. Am. Chem. Soc. 1989, 111, 1082 for further details.

example a

[0242]

[0243] To a solution (200 mL) of m-amino benzoic acid (200 g, 1.46 mol) in concentrated HCl was added an aqueous solution (250 mL) of NaNO2 (102 g, 1.46 mol) at 0° C. The reaction mixture was stirred for 1 h and a solution of SnCl2.2H2O (662 g, 2.92 mol) in concentrated HCl (2 L) was then added at 0° C., and the reaction stirred for an additional 2h at RT. The precipitate was filtered and washed with ethanol and ether to yield 3-hydrazino-benzoic acid hydrochloride as a white solid.

[0244] The crude material from the previous reaction (200 g, 1.06 mol) and 4,4-dimethyl-3-oxo-pentanenitrile (146 g, 1.167 mol) in ethanol (2 L) were heated to reflux overnight. The reaction solution was evaporated in vacuo and the residue purified by column chromatography to yield ethyl 3-(3-tert-butyl-5-amino-1H-pyrazol-1-yl)benzoate (Example A, 116 g, 40%) as a white solid together with 3-(5-amino-3-tert-butyl-1H-pyrazol-1-yl)benzoic acid (93 g, 36%). 1H NMR (DMSO-d6): 8.09 (s, 1H), 8.05 (brd, J...

example b

[0245]

[0246] To a solution of 1-naphthyl isocyanate (9.42 g, 55.7 mmol) and pyridine (44 mL) in THF (100 mL) was added a solution of Example A (8.0 g, 27.9 mmol) in THY (200 mL) at 0° C. The mixture was stirred at RT for 1 h, heated until all solids were dissolved, stirred at RT for an additional 3 h and quenched with H2O (200 mL). The precipitate was filtered, washed with dilute HCl and H2O, and dried in vacuo to yield ethyl 3-[3-t-butyl-5-(3-naphthalen-1-yl)ureido)-1H-pyrazol-1-yl]benzoate (12.0 g, 95%) as a white power. 1H NMR (DMSO-d6): 9.00 (s, 1H), 8.83 (s, 1H), 8.25 7.42 (m, 11H), 6.42 (s, 1H), 4.30 (q, J=7.2 Hz, 2H), 1.26 (s, 9H), 1.06 (t, J=7.2 Hz, 3H); MS (ESI) m / z: 457.10 (M+H+).

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
volumeaaaaaaaaaa
temperatureaaaaaaaaaa
volumeaaaaaaaaaa
Login to View More

Abstract

Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Description

RELATED APPLICATIONS [0001] This application is a continuation-in-part of application Ser. No. 10 / 746,460 filed Dec. 24, 2003 and application Ser. No. 10 / 886,329 filed Jul. 6, 2004. This prior application is incorporated by reference herein. This application also claims the benefit of provisional application entitled Enzyme Modulators for treatment of inflammatory, autoimmune, cardiovascular, and immunological diseases, filed ______. All of the foregoing applications are incorporated by reference herein.BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention relates to novel compounds and methods of using those compounds to treat anti-inflammatory diseases. [0004] 2. Description of the Prior Art [0005] Basic research has recently provided the life sciences community with an unprecedented volume of information on the human genetic code and the proteins that are produced by it. In 2001, the complete sequence of the human genome was reported (Lander, E...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/553A61K31/5377A61K31/4965A61K31/495A61K31/426
CPCC07D231/40C07D401/10C07D401/12C07D403/10C07D403/12C07D405/12C07D409/12C07D413/10C07D417/10C07D417/12C07D453/06
Inventor FLYNN, DANIELPETILLO, PETER
Owner DECIPHERA PHARMA LLC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com